PL2646446T3 - Bromodomain inhibitors and uses thereof - Google Patents
Bromodomain inhibitors and uses thereofInfo
- Publication number
- PL2646446T3 PL2646446T3 PL11844513T PL11844513T PL2646446T3 PL 2646446 T3 PL2646446 T3 PL 2646446T3 PL 11844513 T PL11844513 T PL 11844513T PL 11844513 T PL11844513 T PL 11844513T PL 2646446 T3 PL2646446 T3 PL 2646446T3
- Authority
- PL
- Poland
- Prior art keywords
- bromodomain inhibitors
- bromodomain
- inhibitors
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/20—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
- C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
- C07K14/4702—Regulators; Modulating activity
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Virology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41911910P | 2010-12-02 | 2010-12-02 | |
| US201161451332P | 2011-03-10 | 2011-03-10 | |
| US201161482473P | 2011-05-04 | 2011-05-04 | |
| US201161540788P | 2011-09-29 | 2011-09-29 | |
| US201161540725P | 2011-09-29 | 2011-09-29 | |
| EP11844513.9A EP2646446B1 (en) | 2010-12-02 | 2011-12-02 | Bromodomain inhibitors and uses thereof |
| PCT/US2011/063046 WO2012075383A2 (en) | 2010-12-02 | 2011-12-02 | Bromodomain inhibitors and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PL2646446T3 true PL2646446T3 (en) | 2015-10-30 |
Family
ID=46235164
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PL11844513T PL2646446T3 (en) | 2010-12-02 | 2011-12-02 | Bromodomain inhibitors and uses thereof |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US8796261B2 (en) |
| EP (1) | EP2646446B1 (en) |
| JP (1) | JP5850944B2 (en) |
| KR (1) | KR101871013B1 (en) |
| CN (1) | CN103415525B (en) |
| AR (1) | AR084070A1 (en) |
| AU (1) | AU2011336417B2 (en) |
| BR (1) | BR112013013167B1 (en) |
| CA (1) | CA2818187C (en) |
| CY (1) | CY1116578T1 (en) |
| DK (1) | DK2646446T3 (en) |
| EA (1) | EA022645B1 (en) |
| ES (1) | ES2545117T3 (en) |
| HR (1) | HRP20150858T1 (en) |
| HU (1) | HUE025321T2 (en) |
| IL (1) | IL226331A (en) |
| MX (1) | MX2013006214A (en) |
| NZ (1) | NZ611964A (en) |
| PL (1) | PL2646446T3 (en) |
| PT (1) | PT2646446E (en) |
| RS (1) | RS54175B1 (en) |
| SG (1) | SG190739A1 (en) |
| SI (1) | SI2646446T1 (en) |
| TW (1) | TWI572607B (en) |
| WO (1) | WO2012075383A2 (en) |
| ZA (1) | ZA201303776B (en) |
Families Citing this family (150)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2118074T3 (en) | 2007-02-01 | 2014-03-10 | Resverlogix Corp | Compounds for the prevention and treatment of cardiovascular diseases |
| KR101709492B1 (en) | 2009-03-18 | 2017-02-23 | 리스버로직스 코퍼레이션 | Novel anti-inflammatory agents |
| MX373121B (en) | 2010-05-14 | 2020-04-30 | Dana Farber Cancer Inst Inc | COMPOSITIONS AND METHODS FOR THE TREATMENT OF LEUKEMIA. |
| US9301962B2 (en) | 2010-05-14 | 2016-04-05 | Baylor College Of Medicine | Male contraceptive compositions and methods of use |
| MX384074B (en) | 2010-05-14 | 2025-03-12 | Dana Farber Cancer Inst Inc | COMPOSITIONS AND METHODS FOR TREATING NEOPLASMS, INFLAMMATORY DISEASES AND OTHER DISORDERS. |
| AR084070A1 (en) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | BROMODOMINIUM INHIBITORS AND USES OF THE SAME |
| US9249161B2 (en) | 2010-12-02 | 2016-02-02 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| US8912221B2 (en) * | 2010-12-27 | 2014-12-16 | Hoffmann-La Roche Inc. | Biaryl amide derivatives |
| EP2705039B1 (en) | 2011-05-04 | 2017-07-26 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| US9328117B2 (en) | 2011-06-17 | 2016-05-03 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| WO2013033269A1 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same |
| WO2013033270A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same |
| RU2640115C2 (en) | 2011-11-01 | 2017-12-26 | Ресверлоджикс Корп. | Pharmaceutical compositions of substituted quinazolinones |
| JP2015508414A (en) | 2012-01-12 | 2015-03-19 | イエール ユニバーシティ | Compounds and methods for enhanced degradation of target proteins and other polypeptides by E3 ubiquitin ligase |
| TWI602820B (en) * | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | Bromodomain inhibitors and uses thereof |
| US9624244B2 (en) | 2012-06-06 | 2017-04-18 | Constellation Pharmaceuticals, Inc. | Benzo [B] isoxazoloazepine bromodomain inhibitors and uses thereof |
| WO2013185284A1 (en) * | 2012-06-12 | 2013-12-19 | Abbott Laboratories | Pyridinone and pyridazinone derivatives |
| PE20150729A1 (en) * | 2012-08-16 | 2015-06-14 | Bayer Pharma AG | 2,3-BENZODIAZEPINES |
| HK1208448A1 (en) | 2012-09-28 | 2016-03-04 | Bayer Pharma Aktiengesellschaft | Bet protein-inhibiting 5-aryl triazole azepines |
| WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
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| CA2901352A1 (en) | 2013-02-19 | 2014-08-28 | Bayer Pharma Aktiengesellschaft | Bicyclo 2,3-benzodiazepines and spirocyclically substituted 2,3-benzodiazepines |
| HK1212345A1 (en) | 2013-02-22 | 2016-06-10 | Bayer Pharma Aktiengesellschaft | 4-substituted pyrrolo- and pyrazolo-diazepines |
| JP2016513117A (en) | 2013-02-22 | 2016-05-12 | バイエル ファーマ アクチエンゲゼルシャフト | Pyrrolo- and pyrazolo-triazolodiazepines as BET protein inhibitors for the treatment of hyperproliferative diseases |
| AU2014223990A1 (en) * | 2013-02-28 | 2015-09-10 | Washington University | Methods of treatment of human cytomegalovirus infection and diseases with bromodomain inhibitors |
| EP2970285B1 (en) * | 2013-03-11 | 2019-04-17 | AbbVie Inc. | Fused tetracyclic bromodomain inhibitors |
| JP6401773B2 (en) | 2013-03-11 | 2018-10-10 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | BET bromodomain inhibitor and therapeutic method using the same |
| CN105026403B (en) * | 2013-03-12 | 2018-05-18 | 艾伯维公司 | Tetracyclic Bromodomain Inhibitors |
| WO2014159837A1 (en) * | 2013-03-14 | 2014-10-02 | Convergene Llc | Methods and compositions for inhibition of bromodomain-containing proteins |
| US9714946B2 (en) | 2013-03-14 | 2017-07-25 | Dana-Farber Cancer Institute, Inc. | Bromodomain binding reagents and uses thereof |
| US9227985B2 (en) | 2013-03-15 | 2016-01-05 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| WO2014173241A1 (en) | 2013-04-26 | 2014-10-30 | Beigene, Ltd. | Substituted5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones |
| TWI527811B (en) | 2013-05-09 | 2016-04-01 | 吉李德科學股份有限公司 | Benzimidazole derivatives as bromodomain inhibitors |
| US8975417B2 (en) * | 2013-05-27 | 2015-03-10 | Novartis Ag | Pyrazolopyrrolidine derivatives and their use in the treatment of disease |
| CA2912986A1 (en) * | 2013-05-28 | 2014-12-04 | Novartis Ag | Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease |
| WO2014193951A1 (en) * | 2013-05-28 | 2014-12-04 | Dana-Farber Cancer Institute, Inc. | Bet inhibition therapy for heart disease |
| WO2015004533A2 (en) | 2013-06-21 | 2015-01-15 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| SG11201510409QA (en) | 2013-06-21 | 2016-01-28 | Zenith Epigenetics Corp | Novel bicyclic bromodomain inhibitors |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
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| KR20160037201A (en) * | 2013-08-06 | 2016-04-05 | 온코에틱스 게엠베하 | Method of treating diffuse large b-cell lymphoma (dlbcl) using a bet-bromodomain inhibitor |
| EP3066101B1 (en) | 2013-11-08 | 2020-07-29 | Dana-Farber Cancer Institute, Inc. | Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
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| US10300073B2 (en) | 2014-10-14 | 2019-05-28 | The Regents Of The University Of California | Use of CDK9 and BRD4 inhibitors to inhibit inflammation |
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| JP6788584B2 (en) * | 2014-10-31 | 2020-11-25 | マサチューセッツ インスティテュート オブ テクノロジー | Massively Parallel Combinatorial Genetics on CRISPR |
| WO2016087942A1 (en) | 2014-12-01 | 2016-06-09 | Zenith Epigenetics Corp. | Substituted pyridines as bromodomain inhibitors |
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